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Letters in Drug Design & Discovery

Author(s): E. Bellavance, V. Luu-The and D. Poirier

DOI: 10.2174/1570180043398867

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First Inhibitors of the Steroidogenic Enzyme Type 7 17β-Hydroxysteroid Dehydrogenase

Page: [194 - 197] Pages: 4

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Abstract

We present the SAR study that led us to identification of the first inhibitors of type 7 17β- hydroxysteroid dehydrogenase (17β-HSD). The conversion of E1 into E2 is reduced by nearly 90 % by 17β-(Nalkylformamido)- 4-methyl-4-aza-5α-androstan-3-one compounds bearing a side chain containing 7 to 10 carbon atoms when tested at 0.3 μM.

Keywords: enzyme, hydroxysteroid dehydrogenase, 4-aza-steroids, sar, inhibitors, steroidogenesis